Abstract Thiazole and carbonyl often act as core functional or regulative moieties in biological molecules as well as optical materials. Designing and synthesis of carbonyl‐containing thiazoles are of great importance for related fields, hence, a simple and practical method was developed using commercially xanthates, benzylamine, and readily available alkynones as substrates. The reaction was achieved using one‐pot Michael addition and cascade iodine mediated C−H thiolation under mild conditions. This method features a broad substrate scope with high yield. Remarkably, the obtained carbonyl substituted thiazoles bearing electronic‐donating substituents exhibit promising performance for aggregation‐induced emission (AIE) and have been successfully used in biological imaging.
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